Glaucocalyxin A (hereinafter referred to as GLA), also known as “wangzaozi ne B”, is extracted from the whole part above ground of Rabdosia japonica (Burm.f.) Hara var. glaucocalyx (Maxim.) Hara which belongs to the family labiatae. Glaucocalyxin A has the chemical name of Kaur-16-ene-3,15-dione,(7α, 14R)—, the molecular formula of C20H28O4 and the molecular weight of 332.43, and the structure as shown below:

The content of glaucocalyxin A in dry leaves of the Rabdosia japonica (Burm.f.) Hara var. glaucocalyx (Maxim.) Hara is up to 1.03% [Yuantong Zhang, Dongxu Sha, Ming Sha et al., China Journal of Chinese Materia Medica, 1991, 16 (11):679]. It has a structure similar to oridonin, and belongs to the ent-Kaurane diterpenoids. In its structure, there is also the anti-tumor group, α,β-unsaturated cyclopentanone structural unit, which is similar to oridonin. In vitro and in vivo anti-tumor experiments have shown that it has a significant inhibitory effect on proliferation of various human tumor cell strains (CE-1, U87, A549, MCF-7, Hela, K562, HepG2, NCI-H460, KB, JEG-3, K562, HL-60), especially for the cells of hormone non-dependent prostate cancer (DU-145) and rectal cancer (Lovo), and has a wide range of anti-tumor effects; it can inhibit the growth of solid tumors such as Lewis lung cancer, S180 solid type and HCA solid type and the like, and significantly increase the life extension rate of S180 ascites type and HCA ascites type mice, and the effect of anti-tumor effect is dose-dependent. The recent literature in 2011 [Li WenGao, Jian Zhang, Wen Hua Yang, Bin Wang, Jian Wen Wang. Toxicology in Vitro 2011, 25: 51-63] has reported that glaucocalyxin A can induce apoptosis through mitochondria-regulated death pathway to inhibit the proliferation of human promyelocytic leukemia cell, and thus it is a promising precursor compound with anti-tumor activity.
In addition, as a drug against autoimmune disease, glaucocalyxin A has made a breakthrough in the treatment of systemic lupus erythematosus and psoriasis and the like, and has achieved good therapeutic effect. It has been pointed out in the literature “Research Progress of Rabdosia ameth ystoides(Benth)Hare” [Yu Su, Jia Cui, Wuwu Shi et al., The Asia-pacific Traditional Medicine, 2011, June] that glaucocalyxin A obtained from Rabdosia japonica not only has anti-cancer, anti-bacterial, liver protection and cardiovascular protection effects, but also is active in autoimmune suppression.
However, glaucocalyxin A has a low polarity and poor water solubility, and thus is not suitable for direct administration as a drug; it has strong anti-autoimmune and anti-tumor effects in vitro, while in vivo it requires a large dose and a long time to produce efficacy. It is rapidly cleared in vivo and has a short half-life and a low bioavailability in vivo, and cannot be used directly as a drug yet. Therefore, as an effective way to solve its shortcomings as a drug, under the premise of retaining the active group α,β-unsaturated cyclopentanone, an exocylic double bond is structurally modified to synthesize derivative which has stronger anti-autoimmune and anti-tumor effects.